Anti-inflammatory & anti-allergy agents in medicinal chemistry · 2026
Developing a Natural Oil-Based Organogel to Improve the Topical Delivery of Sertaconazole Nitrate.
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Jain Piyush, Chandrakar Shashikant, Gupta Pushpa Prasad, Pandey Ravindra Kumar, Gidwani Beena
Аннотация
OBJECTIVE: Conventional topical antifungal therapies often exhibit limited efficacy, poor patient adherence, and inadequate stability. To address these challenges, a microwave-assisted clove oil-based organogel of sertaconazole nitrate was developed to enhance antifungal activity, sustain drug release, and improve long-term stability.
METHODS: Organogels were prepared using sertaconazole nitrate, clove oil, Carbopol 934, and polyethylene glycol 400. Physicochemical parameters, including pH, viscosity, spreadability, and drug content, were evaluated, followed by in vitro drug release and ex vivo skin permeation studies using Franz diffusion cells. Antifungal activity was tested against Candida albicans and Trichophyton rubrum, while in vivo therapeutic efficacy and skin irritation were assessed in a dermatophytosis rat model. The long-term stability of the formulation was monitored for 24 months.
RESULTS: The optimized formulation (F12) showed excellent performance, with a drug content of 99.96%, viscosity of 41.45 Pa.s, and spreadability of 26.81 g.cm/sec. Drug release reached 99.5% within 24 hours, following zero-order kinetics with a non-Fickian release mechanism. Ex vivo permeation was significantly higher (99.2%) than that of the marketed cream (81.7%). Enhanced antifungal activity was observed, with inhibition zones of 1.82 cm (Candida albicans) and 2.01 cm (Trichophyton rubrum). In vivo studies confirmed effective therapeutic action without signs of skin irritation. Notably, the formulation maintained its physicochemical integrity and antifungal potency throughout 24 months of storage.
DISCUSSION: The microwave-assisted technique proved to be a simple, reproducible, and efficient approach for organogel fabrication. The inclusion of clove oil contributed to improved antifungal performance and enhanced skin permeation, thereby strengthening the formulation's therapeutic potential.
CONCLUSION: The developed sertaconazole nitrate organogel demonstrated a safe, effective, and stable topical delivery system with superior antifungal efficacy and long-term stability, representing a promising alternative to conventional antifungal therapies.
METHODS: Organogels were prepared using sertaconazole nitrate, clove oil, Carbopol 934, and polyethylene glycol 400. Physicochemical parameters, including pH, viscosity, spreadability, and drug content, were evaluated, followed by in vitro drug release and ex vivo skin permeation studies using Franz diffusion cells. Antifungal activity was tested against Candida albicans and Trichophyton rubrum, while in vivo therapeutic efficacy and skin irritation were assessed in a dermatophytosis rat model. The long-term stability of the formulation was monitored for 24 months.
RESULTS: The optimized formulation (F12) showed excellent performance, with a drug content of 99.96%, viscosity of 41.45 Pa.s, and spreadability of 26.81 g.cm/sec. Drug release reached 99.5% within 24 hours, following zero-order kinetics with a non-Fickian release mechanism. Ex vivo permeation was significantly higher (99.2%) than that of the marketed cream (81.7%). Enhanced antifungal activity was observed, with inhibition zones of 1.82 cm (Candida albicans) and 2.01 cm (Trichophyton rubrum). In vivo studies confirmed effective therapeutic action without signs of skin irritation. Notably, the formulation maintained its physicochemical integrity and antifungal potency throughout 24 months of storage.
DISCUSSION: The microwave-assisted technique proved to be a simple, reproducible, and efficient approach for organogel fabrication. The inclusion of clove oil contributed to improved antifungal performance and enhanced skin permeation, thereby strengthening the formulation's therapeutic potential.
CONCLUSION: The developed sertaconazole nitrate organogel demonstrated a safe, effective, and stable topical delivery system with superior antifungal efficacy and long-term stability, representing a promising alternative to conventional antifungal therapies.